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Hybrid bombesin analogues: combining an agonist and an antagonist in defined distances for optimized tumor targeting
Carsten Kroll1, Rosalba Mansi, Friederike Braun
1Laboratory of Organic Chemistry, ETH Zürich , Zürich, Switzerland.
Abstract:
Radiolabeled hybrid ligands with defined distances between an agonist and an antagonist for the gastrin-releasing peptide receptor were found to have excellent tumor-targeting properties. Oligoprolines served as rigid scaffolds that allowed for tailoring distances of 10, 20, and 30 Å between the recognition elements. In vitro and in vivo studies revealed that the hybrid ligand with a distance of 20 Å between the recognition elements exhibits the highest yet observed tumor cell uptake and retention time in prostate cancer cells.
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